Compositions, methods, and kits useful for the alleviation of gastrointestinal effects

Abstract

Disclosed are compositions, methods, and kits for treating conditions including; ameliorating side effects associated with compounds such as lipase inhibitors; gastrointestinal distress; fecal urgency; obesity; hyperlipidemia; diarrhea; reducing levels of toxic substances; reducing blood cholesterol levels; inducing satiety; effecting weight loss; effecting weight control; and treating, delaying onset and/or preventing Type II diabetes. One embodiment includes compositions for administration to an animal for stiffening lipophilic substances in the gastrointestinal tract. Such stiffening agents have a complete melting point of about 33° C. or greater. Kits comprising the composition are also included. Methods of stiffening lipophilic substances present in the gastrointestinal tract of an animal are also provided. The methods comprise administering a composition comprising a safe and effective amount of a stiffening agent to an animal. The methods also comprise administering a composition comprising a safe and effective amount of a stiffening agent and a safe and effective amount of a lipase inhibitor to an animal.

1. A composition comprising:
 (a) a stiffening agent having a complete melting point of about 33° C. or greater which is selected from the group consisting of R—COOR′, R—OR′, R—CONR′R″, R—NR′R″, salts thereof, and mixtures thereof, wherein:
 (i) R is selected from the group consisting of alkyl radicals having from about 14 to about 24 carbon atoms, alkenyl radicals having from about 14 to about 24 carbon atoms, alkynyl radicals having from about 14 to about 24 carbon atoms, heteroalkyl radicals having from about 14 to about 24 carbon atoms, heteroalkenyl radicals having from about 14 to about 24 carbon atoms, and heteroalkynyl radicals having from about 14 to about 24 carbon atoms; and 
 (ii) R′ and R″ are each, independently, selected from the group consisting of hydrogen, alkyl radicals, alkenyl radicals, alkynyl radicals, heteroalkyl radicals, heteroalkenyl radicals, and heteroalkynyl radicals; and 
 
 (b) a lipase inhibitor; and 
 (c) a non-digestible, non-absorbable, open-celled high internal phase emulsion (HIPE) foam. 
 
     
     
       2. The composition according to  claim 1 , wherein the stiffening agent is selected from the group consisting of fatty acids, salts of fatty acids, and mixtures thereof. 
     
     
       3. The composition according to  claim 2  wherein the lipase inhibitor is selected from the group consisting of 2-amino-4H-3,1-benzoxazin-4-ones; 2-oxy-4H-3,1-benzoxazin-4-ones; 2-thio-4H-3,1-benzoxazin-4-ones; tetrahydrolipstatins; chiral alkylphosphonates; chiral isomers of beta-lactone; and mixtures thereof. 
     
     
       4. The composition according to  claim 3  wherein the lipase inhibitor is a compound selected from the group consisting of tetrahydrolipstatin, lipstatin, and mixtures thereof. 
     
     
       5. The composition according to  claim 4  comprising about 0.001% to about 15% of the lipase inhibitor and about 0.1% to about 99% of the stiffening agent, all by weight of the composition. 
     
     
       6. The composition according to  claim 2  comprising about 0.2% to about 95% of the stiffening agent, by weight of the composition. 
     
     
       7. The composition according to  claim 6  comprising about 0.8% to about 95% of the stiffening agent, by weight of the composition. 
     
     
       8. The composition according to  claim 7  wherein the lipase inhibitor is tetrahydrolipstatin. 
     
     
       9. The composition according to  claim 7  wherein the stiffening agent is selected from the group consisting of calcium stearate, behenic acid, and mixtures thereof.